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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
27 Results for "
DYRK1A/B
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "DYRK1A/B" in MCE Product Catalog:
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4 Cited Publications
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
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2 Cited Publications
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
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2 Cited Publications
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EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis - .
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Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research .
1
1 Cited Publications
Synonyms: Mirk-IN-1; DYRK1B/A-IN-1
RO5454948 (Compound 9) is the inhibitor for Dyrk1B and Dyrk1A with IC50 of 68 nM and 22 nM. RO5454948 exhibits cytotoxicity in cancer cell SW620 with EC50 of 1.9 μM .
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1 Cited Publications
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Dyrk1A-IN-5 (Compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC50 = 600 nM) and CLK1 (IC50 = 500 nM), but shows almost no inhibition of DYRK2 (IC50 > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research .
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1 Cited Publications
Cat. No.: HY-X0009A
CAS No.: 2559759-04-3
Synonyms: GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate
Research Areas:
Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research .
Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3) .
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EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively .
Synonyms: 108600
Research Areas:
ON 108600 (108600) is a CK2 (CK2α1: IC50 = 50 nM; CK2α2 = 5 nM), TNIK (IC50 = 5 nM) and DYRK (DYRK1A: IC50 = 16 nM; DYRK1B = 7 nM; DYRK2: = 28 nM). ON 108600 suppresses the growth of CD44high/CD24low breast cancer stem cell (BCSC) populations, induces G2/M arrest and apoptosis in triple negative breast cancer (TNBC) cells, and inhibits tubulin polymerization. ON 108600 can be used for the study of chemotherapy-resistant and metastatic TNBC .
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Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .
Cat. No.: HY-144614
CAS No.: 3034312-17-6
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JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
Cat. No.: HY-146337
CAS No.: 3032401-50-3
Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable DYRK1A and DYRK1B inhibitor with Kis of 67.8 nM and 237.9 nM, and IC50s of 1.1 μM and 0.8 μM, respectively. Dyrk1A/B-IN-1 is not toxic to human cells. Dyrk1A/B-IN-1 can be used for researching DYRK1A and DYRK1B cellular functions and their role in pathologies .
Cat. No.: HY-144617
CAS No.: 2426628-29-5
JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines .
Cat. No.: HY-128759
CAS No.: 1386980-04-6
DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity .
Cat. No.: HY-128758
CAS No.: 1387090-01-8
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .
Cat. No.: HY-159496
CAS No.: 2891824-14-7
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Dyrk1A-IN-10 (compound B4) is a DYRK1A inhibitor with antidiabetic activity. Dyrk1A-IN-10 can promote pancreatic β-cell proliferation, increase insulin secretion, and lower blood sugar .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
